.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 5,965,168

« Back to Dashboard

Claims for Patent: 5,965,168

Title: Microencapsulated 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
Abstract:The invention relates to a pharmaceutical composition comprising a biodegradable and biocompatible microparticle composition comprising a 1,2-benzazole of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, within a polymeric matrix.
Inventor(s): Mesens; Jean (Wechelderzande, BE), Rickey; Michael E. (Loveland, OH), Atkins; Thomas J. (York, PA)
Assignee: Alkermes Controlled Therapeutics, Inc. II (Cambridge, MA) Janssen Pharmaceutica (BE)
Application Number:09/005,549
Patent Claims: 1. A sustained-release microparticle comprising: a 1,2-benzazole of the formula ##STR16## and the pharmaceutically acceptable acid addition salts thereof, wherein R is hydrogen or alkyl of 1 to 6 carbon atoms;

R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen, halo, hydroxy, alkyloxy of 1 to 6 carbon atoms, and C alkyl of 1 to 6 carbon atoms;

X is O or S;

Alk is C.sub.1-4 alkanediyl; and

Q is a radical of formula ##STR17## wherein R.sup.3 is hydrogen or alkyl of 1 to 6 carbon atoms;

Z is --S--, --CH.sub.2 --, or --CR.sup.4 .dbd.CR.sup.5 --; where R.sup.4 and R.sup.5 are independently selected from the group consisting of hydrogen or alkyl of 1 to 6 carbon atoms;

A is a bivalent radical --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or CR.sup.6 .dbd.CR.sup.7 --;

where R.sup.6 and R.sup.7 are independently selected from the group consisting of hydrogen, halo, amino or alkyl of 1 to 6 carbon atoms; and

R.sup.8 is hydrogen or hydroxyl; and a biodegradable and biocompatible polymeric matrix.

2. The sustained-release microparticle of claim 1, wherein the biodegradable and biocompatible polymeric matrix is selected from the group consisting of poly(glycolic acid), poly-D,L-lactic acid, poly-L-lactic acid, copolymers of the foregoing, poly(aliphatic carboxylic acids), copolyoxalates, polycaprolactone, polydioxonone, poly(ortho carbonates), poly(acetals), poly(lactic acid-caprolactone), polyorthoesters, poly(glycolic acid-caprolactone), polyanhydrides, albumin, casein, and waxes.

3. The sustained-release microparticle of claim 1, wherein said 1,2-benzazole comprises 1 to 90 wt. % of the microparticle.

4. The sustained-release microparticle of claim 1, wherein said 1,2-benzazole comprises about 35 to 40 wt. % of the microparticle.

5. The sustained-release microparticle of claim 1, wherein the microparticle ranges in size from 1 to 500 microns.

6. The sustained-release microparticle of claim 1, wherein the microparticle ranges in size from 25 to 180 microns.

7. The sustained-release microparticle of claim 1, wherein the microparticle is formulated in a liquid injection vehicle.

8. The sustained-release microparticle of claim 7, wherein said liquid injection vehicle is selected from the group consisting of

A. physiological saline solution and

B. an aqueous solution of carboxymethyl cellulose with a surfactant.

9. The sustained-release microparticle of claim 1, wherein the microparticle is administered by intramuscular injection.

10. The sustained-release microparticle of claim 1, wherein the microparticle is administered by subcutaneous injection.

11. The sustained-release microparticle of claim 1, wherein the 1,2-benzazole is selected from the group consisting of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl)ethyl]-6,7,8,9-tetr ahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one and the pharmaceutically acceptable acid addition salts thereof.

12. The sustained-release microparticle of claim 1, wherein the 1,2-benzazole is selected from the group consisting of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl)ethyl]-6,7,8,9-tetr ahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one and the pharmaceutically acceptable acid addition salts thereof.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc